P-糖蛋白抑制剂维拉帕米对龙血素A、B、C在大鼠体内药物动力学影响

研究灌胃给予大鼠龙血竭后,P糖蛋白抑制剂维拉帕米对其有效成分龙血素A、B、C在大鼠血浆中的药物动力学影响.将SD大鼠随机分为对照组和抑制剂组并单次给药,对照组灌胃给予大鼠5 g/kg龙血竭,抑制剂组联合给予大鼠维拉帕米（1 mg/kg）和龙血竭（5 g/kg）.收集两组相同系列时间的血浆样本,采用HPLC-MS/MS的方法对龙血素A、B、C在大鼠血浆中的浓度测进行检测,求算两组血浆样本药物动力学参数.与对照组相比,抑制剂组大鼠龙血素A、B、C的血药浓度-时间曲线下面积分别增加109.4%,78.5%,22.8%,血药峰浓度分别增加69.6%,115.0%,42.1%,龙血素A、B的达峰时间均延长、龙血素C的达峰时间无变化,三者的生物半衰期（T_0.5）均变小,说明P糖蛋白抑制剂能够引起龙血素A、B、C在大鼠体内的血浆药物动力学参数变化,龙血素A、B、C均有可能为P糖蛋白的潜在底物. 

Effect of P-Glycoprotein Inhibitor Verapamil on Pharmacokinetics of Loureirin A B C in Rats

To study how P-glycoprotein inhibitor verapamil affect pharmacokinetics of the active constituents Loureirin A, B and C in rat plasma after oral administration of Dragon''s Blood,SD rats were randomly put into different group:control group and inhibitor group. A single dose of 5 g/kg of Dragon''s Blood was orally administered to rats in control group, and rats in the inhibitor group were given verapamil (1 mg/kg) and Dragon'' Blood (5 g/kg). Plasma samples were collected from the two groups in the same series of time. A HPLC-MS/MS method was used to determine the content of Loureirin A, B and C in rat plasma, and the plasma samples pharmacokinetic parameters were calculated. Comparing the area under curve (AUC0-t) of the rats in the inhibitor group with the control group, it increased by 109.4%,78.5%, 22.8%. And the peak concentration(C_max) of Loureirin A, B and C increased by 69.6%, 115.0%, and 42.1%. The time of Loureirin A and B reaching peak concentration (t_max) was prolonged, while the t_max of Loureirin C was unchanged. All three biological half-life (t_0.5) decreased. It indicates that P-glycoprotein inhibitor can significantly change the plasma pharmacokinetic parameters of Loureirin A, B and C in rats. Loureirin A, B and C may be potential substrates of P-glycoprotein. This article provides basic data for the subsequent in-depth study of the relationship between P-glycoprotein and transportation of Dragon''s Blood in the intestinal tract of rats.